This invention relates to a film-coated extended release oral dosage composition containing the nasal decongestant pseudoephedrine in a unique polymer matrix core and a film-coating on such core containing the non-sedating antihistamine, loratadine. The oral dosage composition is useful for treating patients showing the signs and symptoms associated with upper respiratory diseases and nasal congestion.
Loratadine is disclosed in U.S. Pat. No. 4,282,233 as a non-sedating antihistamine and it is useful as an anti-allergy agent in, for example, the treatment of seasonal allergic rhinitis symptoms such as sneezing and itching.
Pseudephedrine as well as pharmaceutically acceptable acid additional salts, e.g., those of HCl or H.sub.2 SO.sub.4, is a sympathomimetic drug recognized by those skilled in the art as a safe therapeutic agent effective for treating nasal congestion and is commonly administered orally and comcomitantly with an antihistamine for treatment of nasal congestion associated with allergic rhinitis. For example, 5 mg of loratadine and 120 mg of pseudoephedrine sulfate ("PES") in a matrix core repetab tablet product is available wherein the PES is equally distributed in the tablet coating and barrier core and all the loratadine is in the coating. The product is recommended for twice-a-day dosing for effectiveness. It would be desirable to have a once-a-day loratadine-pseudoephedrine product.
The successful development of a formulation of a loratadine-pseudoephedrine once-a-day product requires achieving a release rate profile for pseudoephedrine component over an extended period in excess of twelve hours while maintaining the safety and effectiveness of loratadine. Products containing non-sedating antihistamines in combination with pseudoephedrine such as Seldane-D, a press-coated product of terfenadine and pseudoephedrine and Hismanal-D, a combination of pseudoephedrine prills and a separate astemizole tablet are known. However, the administration of terfenadine and astemizole products to humans has been found to cause adverse effects including cardiac arrhythmias and occurrence of these arrhythmias have increased when the terfenadine or astemizole products are co-administered with other drugs such as ketoconazole and erythromycin or upon overdose of the non-sedating anti-histamine.
It would be desirable for increased patient compliance to have an extended release product effective and safe when used on a once-a-day basis.